casdatifan (AB521)

Casdatifan has shown promising clinical activity in the ARC-20 ccRCC platform study, both as monotherapy and in combination with the VEGFR tyrosine kinase inhibitor (TKI) cabozantinib. Currently, casdatifan is being evaluated in a Phase 3 trial in combination with cabozantinib (NCT07011719) in patients with advanced ccRCC.

These features translated into improved biochemical and cellular activity, including inhibition of hypoxia-regulated gene expression. Insights from this campaign ultimately informed the discovery of casdatifan, a clinical-stage HIF-2α inhibitor, underscoring the translational potential of this novel chemotype.

P2, N=32, Recruiting, Dana-Farber Cancer Institute | Not yet recruiting --> Recruiting | Initiation date: Jul 2026 --> Mar 2026

P1, N=362, Recruiting, Arcus Biosciences, Inc. | Trial completion date: Jul 2027 --> Mar 2029 | Trial primary completion date: Jul 2027 --> Mar 2029

P2/3, N=308, Recruiting, Arcus Biosciences Inc.

P2, N=32, Not yet recruiting, Dana-Farber Cancer Institute

P3, N=1116, Active, not recruiting, AstraZeneca | Recruiting --> Active, not recruiting

P1, N=14, Completed, Arcus Biosciences, Inc. | Active, not recruiting --> Completed

P3, N=720, Recruiting, Arcus Biosciences, Inc. | Not yet recruiting --> Recruiting

P1, N=14, Active, not recruiting, Arcus Biosciences, Inc. | Recruiting --> Active, not recruiting

P3, N=1116, Recruiting, AstraZeneca | Not yet recruiting --> Recruiting

Casdatifan, after single and multiple dosing in healthy participants, was safe and tolerable. Linear PK was associated with a mean maximum erythropoietin reduction of 85% following a single dose and multiple doses of casdatifan, demonstrating a promising exposure-biological activity profile.